New N-arachidonoylserotonin analogues with potential “dual” mechanism of action against pain

…, E Morera, F Rossi, A Schiano-Moriello…

Index: Ortar, Giorgio; Cascio, Maria Grazia; De Petrocellis, Luciano; Morera, Enrico; Rossi, Francesca; Schiano-Moriello, Aniello; Nalli, Marianna; De Novellis, Vito; Woodward, David F.; Maione, Sabatino; Di Marzo, Vincenzo Journal of Medicinal Chemistry, 2007 , vol. 50, # 26 p. 6554 - 6569

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Citation Number: 46

Abstract

N-Arachidonoylserotonin (AA-5-HT, 1a) is an inhibitor of fatty acid amide hydrolase (FAAH) that acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels and is analgesic in rodents. We modified the chemical structure of 1a with the aim of developing “hybrid” FAAH/TRPV1 blockers more potent than the parent compound or obtaining analogues with single activity at either of the two targets to study the mechanism ...